7734-05-6Relevant articles and documents
Synthesis of 6-Oxo-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizine
Tompkins, David C.,Reilly, Laurence W.,Nelson, Randall B.,Dolby, Lloyd J.,Gribble, Gordon W.
, p. 1048 - 1052 (2018/04/24)
An efficient synthesis of 6-oxo-1,2,3,4,5,7,12,12b-octahydroindolo[2,3-α]quinolizine from 2-acetylpyridine and phenylhydrazine is described. This derivative of the natural alkaloid desbromoarborescidine A is an important entry point to the sarpagine-vobas
Synthesis of 7-Oxo-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizine
Tompkins, David C.,Nelson, Randall B.,Dolby, Lloyd J.,Gribble, Gordon W.
, p. 2168 - 2171 (2018/08/03)
A short synthesis of 7-oxo-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizine from 2-acetylpyridine and phenylhydrazine is described. Ring C is forged using 2-chloro-N,N-dimethylacetamide. This derivative of the natural alkaloid 1,2,3,4,6,7,12,12b-octah
Amide derivative, preparation method of amide derivative, and application of amide derivative to pharmacy
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Paragraph 0166-0170, (2017/08/30)
The invention provides an amide derivative, a preparation method of the amide derivative, and application of the amide derivative to pharmacy. The amide derivative compound is selected from one of the following structures. The compound can be used for preparing medicines in the fields of local anaesthesia or analgesia. (The formulas are as shown in the description).
Preparation and characterization of terdentate [C,N,N] acetophenone and acetylpyridine hydrazone platinacycles: A DFT insight into the reaction mechanism
Marcos, Ismael,Ojea, Vicente,Vázquez-García, Digna,Fernández, Jesús J.,Fernández, Alberto,López-Torres, Margarita,Lado, Jorge,Vila, José M.
supporting information, p. 16845 - 16860 (2017/12/26)
The reaction of N-ortho-chlorophenyl-substituted acetylpyridine hydrazones (a and d) with K2[PtCl4] (n-butanol/water, 100 °C) gave mononuclear complexes 1a and 1d with the ligands as [N,N] bidentate. In contrast, the reaction of N-phenyl or N-meta-chlorophenyl hydrazones (b and c, respectively) under analogous reaction conditions gave the cycloplatinated species 2b and 2c with the ligand as [C,N,N] terdentate. The treatment of the mononuclear complexes 1a and 1d with NaOAc (n-butanol, 100 °C) gave the corresponding cycloplatinated complexes 2a and 2d. Acetophenone hydrazone platinacycle 2e was prepared in a similar fashion and its reaction with tertiary mono- and triphosphines gave mono- or trinuclear species depending on the reaction conditions. The X-ray crystal structures of some of these complexes showed interesting π-π slipped stacking interactions between metallacyclic rings which, according to NCI analyses, showed an aromatic character. With an aim to rationalize the different reactivities shown by acetylpyridine hydrazones and the precise role of the acetate anion, the energy profiles for the three main steps of cycloplatination (iminoplatinum complex formation, chelation and cyclometallation) have been determined by using the DFT (M06) methods. Calculations indicate that the cycloplatination of 1b proceeds via electrophilic substitution, involving the direct replacement of the chloride anion at the Pt(ii) centre with the N-phenyl moiety as the rate-determining step, to give an agostic intermediate 5b+ that, subsequently, leads to the elimination of a proton as hydrogen chloride. When present as an external base, acetate enters the coordination sphere around the Pt(ii) centre and facilitates hydrazone N-H deprotonation and electrophilic C-H activation through a dissociative route, leading to a Wheland-type σ-complex intermediate 9ac.
Benzyl Piperidine Compounds as Lysophosphatidic Acid (LPA) Receptor Antagonist
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Paragraph 0107, (2015/02/18)
The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives
Fadda, Ahmed A.,El-Mekawy, Rasha E.,El-Shafei, Ahmed I.
, p. 753 - 768 (2015/10/29)
This manuscript describes the synthesis of a new series of porphyrin structures 4a-4m, 7, 9, 12 and 14. These structures were investigated against two types of viruses such as HIV-1 and HSV-1. Also they were screened for their antitumor activity. Among all tested compounds, it was found that compound 4b showed a high activity against HIV-1 and HSV-1 and against four different tumor cell lines. Most of the tested compounds showed a moderate degree of a potent antimicrobial activity. The structure of these compounds was confirmed on the basis of their analytical and spectral data such as UV-vis, IR, 13C NMR, 1H NMR spectroscopy and mass spectral data.
Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives
Fadda, Ahmed A.,El-Mekawy, Rasha E.,El-Shafei, Ahmed I.
, p. 753 - 768 (2016/01/09)
This manuscript describes the synthesis of a new series of porphyrin structures 4a-4m, 7, 9, 12 and 14. These structures were investigated against two types of viruses such as HIV-1 and HSV-1. Also they were screened for their antitumor activity. Among all tested compounds, it was found that compound 4b showed a high activity against HIV-1 and HSV-1 and against four different tumor cell lines. Most of the tested compounds showed a moderate degree of a potent antimicrobial activity. The structure of these compounds was confirmed on the basis of their analytical and spectral data such as UV-vis, IR, 13C NMR, 1H NMR spectroscopy and mass spectral data.
Microwave effects in organic synthesis: Myth or reality?
Kappe, C. Oliver,Pieber, Bartholomaeus,Dallinger, Doris
supporting information, p. 1088 - 1094 (2013/03/13)
It's not magic! The effects observed in microwave-irradiated chemical transformations can in most cases be rationalized by purely bulk thermal phenomena associated with rapid heating to elevated temperatures. As discussed in this Essay, the existence of s
BENZYL PIPERIDINE COMPOUNDS AS LYSOPHOSPHATIDIC ACID (LPA) RECEPTOR ANTAGONIST
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Page/Page column 18; 19, (2013/04/13)
The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
Fast hydrazone reactants: Electronic and acid/base effects strongly influence rate at biological pH
Kool, Eric T.,Park, Do-Hyoung,Crisalli, Pete
supporting information, p. 17663 - 17666 (2014/01/06)
Kinetics studies with structurally varied aldehydes and ketones in aqueous buffer at pH 7.4 reveal that carbonyl compounds with neighboring acid/base groups form hydrazones at accelerated rates. Similarly, tests of a hydrazine with a neighboring carboxylic acid group show that it also reacts at an accelerated rate. Rate constants for the fastest carbonyl/hydrazine combinations are 2-20 M-1 s-1, which is faster than recent strain-promoted cycloaddition reactions.
